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Lapaquistat acetate and ezetimibe
Lapaquistat acetate and ezetimibe is a Cholesterol absorption inhibitor combination Small molecule drug developed by Takeda. It is currently in Phase 3 development for Hypercholesterolemia / elevated LDL cholesterol. Also known as: TAK-475, Zetia.
Lapaquistat acetate inhibits ACAT2 (acyl-CoA:cholesterol acyltransferase 2) to reduce intestinal cholesterol absorption, while ezetimibe blocks NPC1L1 to further decrease cholesterol uptake, together lowering LDL cholesterol.
Lapaquistat acetate inhibits ACAT2 (acyl-CoA:cholesterol acyltransferase 2) to reduce intestinal cholesterol absorption, while ezetimibe blocks NPC1L1 to further decrease cholesterol uptake, together lowering LDL cholesterol. Used for Hypercholesterolemia / elevated LDL cholesterol.
At a glance
| Generic name | Lapaquistat acetate and ezetimibe |
|---|---|
| Also known as | TAK-475, Zetia |
| Sponsor | Takeda |
| Drug class | Cholesterol absorption inhibitor combination |
| Target | ACAT2 and NPC1L1 |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | Phase 3 |
Mechanism of action
Lapaquistat acetate is an ACAT2 inhibitor that reduces cholesterol esterification in the intestine, decreasing cholesterol absorption. Ezetimibe is an NPC1L1 inhibitor that blocks cholesterol uptake at the intestinal brush border. The combination targets complementary pathways in intestinal cholesterol homeostasis to achieve additive LDL-lowering effects.
Approved indications
- Hypercholesterolemia / elevated LDL cholesterol
Common side effects
- Gastrointestinal effects (diarrhea, constipation)
- Elevated liver enzymes
- Muscle-related symptoms
Key clinical trials
- Efficacy of Lapaquistat Acetate Alone and With Ezetimibe in Subjects With Primary Dyslipidemia. (PHASE3)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Lapaquistat acetate and ezetimibe CI brief — competitive landscape report
- Lapaquistat acetate and ezetimibe updates RSS · CI watch RSS
- Takeda portfolio CI
Frequently asked questions about Lapaquistat acetate and ezetimibe
What is Lapaquistat acetate and ezetimibe?
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Related
- Drug class: All Cholesterol absorption inhibitor combination drugs
- Target: All drugs targeting ACAT2 and NPC1L1
- Manufacturer: Takeda — full pipeline
- Therapeutic area: All drugs in Cardiovascular
- Indication: Drugs for Hypercholesterolemia / elevated LDL cholesterol
- Also known as: TAK-475, Zetia
- Compare: Lapaquistat acetate and ezetimibe vs similar drugs
- Pricing: Lapaquistat acetate and ezetimibe cost, discount & access